摘要 |
The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g. benzyl bromide or a derivative thereof.
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申请人 |
INFLAZYME PHARMACEUTICALS LIMITED;LAUENER, RONALD, W.;BURGOYNE, DAVID, L.;REBSTEIN, PATRICK, J.;MACKENZIE, LLOYD, F.;ZHOU, YUANLIN;SHEN, YAPING |
发明人 |
LAUENER, RONALD, W.;BURGOYNE, DAVID, L.;REBSTEIN, PATRICK, J.;MACKENZIE, LLOYD, F.;ZHOU, YUANLIN;SHEN, YAPING |